Saccharin-The Birth of a Sweet Problem: In 1879, the first artificial sweetener (AS), saccharin, was produced. It was made with the concerted efforts of Dr. Ira Remsen, who later became the second president of Johns Hopkins, and fellow researcher Constantine Fahlberg. They used Toluene, a versatile chemical that is used for dissolving paint, making silicone sealants and increasing octane levels in gas (1). Saccharin is 500 times sweeter than sugar, but more importantly it paved the way for more AS to unfortunately make its way into our food supply.

What are artificial sweeteners? They are just that, artificial. They are not found in nature, they are not involved with the rebuilding or repairing process nor are they involved or needed in our growth and development. In fact, they have no place in human physiology or biochemistry. With that said these AS are not just in our marketplaces but are thriving. Why then do these chemical sweeteners do so well? The reason is multifactorial. Their success comes from the following:

Advertising and marketing: AS are positioned as the alternative to sugar. We know that sugar consumption leads to weight gain and is the central ingredient in contracting Type 2 diabetes. Since sugar is harmful to our health, we are led to believe that these sugar substitutes, are, by default, safe and beneficial.

Taste: AS are much sweeter than table sugar. Some AS are hundreds or even thousands of times sweeter than table sugar. This only expedites our cravings for them.

No calories: AS contain no calories, which can be interpreted as beneficial for the people who are trying to lose weight since 3,500 calories equals a pound of fat.

Cheap to produce: Since AS are chemically engineered they can be produced in an unlimited supply. There is no need to grow, farm or maintain anything.

Availability: AS are presented in those pretty pink, yellow and blue packets and are always in arm’s reach anywhere food or coffee is sold. They are also in thousands of food products that we may not associate with sweets.

Approval from the Government: Finally, the government, which not only allowed these AS to be unleashed to the public but also endorsed them by giving them “generally regarded as safe” (GRAS) status.

When you have these powerful influences converging on an unsuspecting public it becomes a recipe for disaster. This is especially true for the diabetic, the overweight or any person trying to lose weight who are more apt to use AS thinking that they are a safe substitute. The problem with AS extends well past the sugar-overweight connection. Stated below is a thumbnail perspective of some of the most promoted AS along with a more accurate depiction of their safety.

Cyclamate-Saccharin’s Little Banned Brother:In 1937, the second marketed AS, cyclamate, was produced. It was engineered by graduate student Michael Sveda who was designing an anti-fever drug. This AS was rated 500 times sweeter than sugar. Cyclamate had the properties of being water soluble, heat stable, cheap to produce, and didn’t have the extensive metallic after-taste as its predecessor. In other words, perfect for mass production. In 1958, both saccharin and cyclamate received GRAS status by the Food Additives Amendment to the Food, Drug and Cosmetic Act (1). However, in 1969, cyclamate was taken off the market as it produced bladder cancer in laboratory mice. I guess the mice tested for cyclamate in 1958 were just healthier.

Aspartame (Equal and NutraSweet) – A Very Exciting Artificial Sweetener
In 1965, the third marketed AS was produced by scientist James Schlatter. He was designing an ulcer medication when he produced the AS, aspartame. Unlike its two predecessors, aspartame (shown right) is metabolized by the body. Aspartame is made up of two amino acids and a methyl ester. The two amino acids are phenylalanine and aspartic acid.

Amino acids are the building blocks of protein and there are 22 known amino acids, ten of which are essential. Amino acids play an enormous role in our physiology including building muscle, whereby aspartame gets marketed and praised as not just being “safe” but also “beneficial”. This, of course, like the other AS commercials are cleverly deceitful and purposely misleading. Let’s review why. Amino acids in food (e.g. meat, fish, poultry, eggs) come packaged in relative proportion to each other. There are no foods that contain just two amino acids, as does aspartame. Secondly, there are no foods containing 50% phenylalanine or 40% aspartic acid. Food containing the essential amino acid phenylalanine may be as high as 4-5%, not 50% as in aspartame and in terms of aspartic acid it is a non-essential amino acid anyway (2). Let’s also remember that amino acids readily cross the blood brain barrier (BBB) and therefore directly affect brain chemistry.

Phenylalanine metabolizes into tyrosine, l-dopa, norepinephrine and epinephrine which are either precursors to, or are neurotransmitters. These neurotransmitters compete with other neurotransmitters and in the case of phenylalanine, it competes with the amino acids tryptophan and serotonin. High doses of phenylalanine will competitively inhibit tryptophan and serotonin. A deficiency of tryptophan and serotonin results in loss of sleep, anxiety and depression (3). Just to note: There is a small population who lack the enzyme phenylalanine hydroxylase and cannot take phenylalanine anyway; it is a condition known as phenylketonuria (PKU).

Aspartic acid, the other amino acid in aspartame, is a major excitatory amino acid. It works similarly to monosodium glutamate (MSG). Being a major excitatory amino acid, aspartic acid increases synaptic firing between neurons which leads to free radical damage, oxidative damage, and neuronal death. The increased firing of excitatory neurotransmitters leads to the exhaustion and ultimately the death of neurons. It is well accepted that this mechanism serves as a catalyst to neurodegenerative pathology like Parkinson’s and Alzheimer’s disease and other dementias (3). Seizures and strokes occur from this mechanism as well; and with a 40% dosing load of aspartic acid per aspartame packet, it clearly plays a major role. More of the common findings from high level excitation include headaches, eye pain and light sensitivity. That is the effect excitotoxins (a term coined by neuroscientist Dr. John Olney) have on the brain (3).

If having these two amino acids circulate disproportionately and freely throughout the blood stream and into the BBB doesn’t convince you to avoid aspartame, perhaps looking at its third and final ingredient, methyl ester, will. Once consumed, the methyl ester gets cleaved off the aspartame structure and forms methanol, also known as wood alcohol, a poison.

There is a vast difference between methanol and ethanol (the alcohol we consume). Structurally methanol contains one carbon while ethanol contains two carbons. Ethanol when consumed gets metabolized in the liver by the P450 cytochrome system; it also undergoes further metabolism and forms acetyl CoA which enters the Kreb’s Acid Cycle. When ethanol is taken in amounts that the body metabolizes before it accumulates, ethanol consumption can be safe. However, methanol is a different story. Methanol is extremely difficult to metabolize and, as such, accumulates and marinates throughout the body causing further destruction. Methanol breaks down into formaldehyde and formic acid, both of which are highly toxic and dangerous to our body and destructive to the optic nerve and retina. Formaldehyde is an embalming substance that is 5,000 times more potent than ethanol and also disrupts DNA which leads to cancer (1). Formic acid, the other metabolite, is six times more toxic than methanol (4). Since both metabolites have a destructive affinity to visual function, consumers of aspartame may suffer headaches, visual disturbances and impairment including blindness. Formaldehyde and formic acid are used in over 200 industrial and household products including antifreeze, carpets, paint solvents, plastics, to name a few. Methanol should never be consumed; it’s been estimated that two undiluted teaspoons in a child or a quarter of a cup in an adult would likely result in death (4).

Methanol also has a place in American history. When the Eighteenth Amendment, also known as Prohibition, of the United Stated Constitution took effect in January 1920, for the purpose of prohibiting the production, sale and transport of alcohol, methanol reared itself. Prohibition seemed like a noble idea, as the government felt that they could legislate behavior by limiting alcohol consumption. This plan was a catastrophe. As a consequence, Prohibition actually caused an increase in people drinking (4). Secondly, it also brought forth organized crime who capitalized by producing and distributing bootleg liquor. The alcohol used was methanol. Methanol is produced by distilling wood products like sawdust, lumber, or furniture and hence, the name wood alcohol. Methanol fit the bill perfectly since it was very cheap to make and its taste was indistinguishable from grain-based ethanol. Since methanol was slow to metabolize its deleterious effects didn’t take place for about a week (5). The effects from methanol consumption ranged from blurry vision, acute nausea, to seizures, blindness, coma and even death. As Prohibition continued, the government remained steadfast in their “noble” cause and decided to denature any alcohol not used for drinking purposes therefore producing a stronger poison. The chemicals used included methanol, formaldehyde (a byproduct of methanol), benzene, ether, cadmium and gasoline (5). Furthermore, the government issued warnings to the dangers of consuming denatured alcohol, something they were part of. Despite being the law, or being constantly warned, or risking health, including the loss of life, the committed drinker remained dedicated to drinking.

In December of 1933, the Twenty-first Amendment was now in effect. Its sole purpose was repealing the Eighteenth Amendment, the only amendment to have that distinction. The reason Prohibition was repealed wasn’t due to the tragedy it had on human life, although that should have been enough since there was more loss of life in a year’s period than from the entire World War I (5), but rather due to the development of organized crime and a major loss of tax revenue (bingo) to the government.

The point is that methanol was used by both the bootleggers and the government, however, for different reasons. Today, the government has the Food and Drug Administration (FDA), whose duty and responsibility is to supervise food safety while protecting and promoting public health, but ironically has allowed the poisonous methanol in AS to be sold freely in the open market; at least during Prohibition warnings were given about its dangers.

Additional studies on aspartame and methanol show that methanol caused holes in the brain of rats, and in 1967, a study on seven monkeys using aspartame resulted in the death of one monkey while five others suffered grand mal seizures (1,2).

When aspartame was unleashed for public consumption there were more complaints sent to the FDA than any other AS. These findings included tinnitus, dizziness, heart palpitations, tachycardia, brain tumors, diabetes, arthritis, Parkinson’s and Alzheimer’s disease along with the usual headaches and visual problems (1,2).

A salient side note, another AS, Neotame, which is 7,000-13,000 times sweeter than table sugar, is a modified version of aspartame. Neotame (shown right), is basically aspartame with a neohexyl group added. However, the advertisers framed neotame as safer than aspartame because when it was metabolized, the phenylalanine in neotame isn’t broken off in free-form as it is with aspartame, and therefore “safe” for people with PKU. Of course neotame is far from being safe as it only keeps one’s addiction to sweets intact while still allowing methanol to circulate freely throughout the bloodstream (6).

Sucralose is dangerous for the following reasons. As stated earlier, sucralose came about by altering the disaccharide, sucrose. All disaccharides must contain at least one glucose molecule. In the case of sucrose, there is one glucose and one fructose sugar to make it a disaccharide. However, in making sucralose both sugars of sucrose were altered leaving no glucose available, resulting in a foreign “disaccharide” which our body simply cannot utilize for any physiological purpose, regardless of how sweet it is, or how addicted we become to it.

Sucralose contains chlorine. Chlorine is a highly reactive gas that doesn’t exist in nature but can be artificially produced through the electrolysis of sodium chloride. There is also a vast difference between chlorine and chloride, just as there is a difference, as Mark Twain put it, between lightning and a lightning bug. Chloride exists as an ion that reacts with sodium to produce sodium chloride (table salt), which is compatible with our physiology. The bond that is formed between these two elements is an ionic bond which is based upon electrostatic attraction. Chlorine, on the other hand, is chemically manipulated to form a covalent bond with carbon. The covalent bond is based upon sharing and is a more stable bond than the ionic bond. The chlorine-carbon bond is also known as an organochlorine or a chlorocarbon and is not compatible in human physiology. Members of the organochlorine family include the insecticides DDT, Dicofol, Methoxychlor, Chlorodane, and Trans-Nonachlor, the carcinogen Dioxin, the anesthetic chloroform, the banned fungicide Hexachlorobenzene (HCB), the electrical insulator Polychlorinated Biphenyls (PCBs), the chemical warfare agents mustard gas and phosgene, just to name a few. There has only been one organochlorine ever used for human consumption,and that is sucralose. The Environmental Protection Agency (EPA) has also classified chlorine as a class-one carcinogen (cancer causing agent) (1). Therefore the difference between chloride and chlorine is the difference between food and poison.

The way these organochlorines work is that the organic component, carbon, serves as a carrier where it allows the highly reactive, deleterious chlorine to freely enter into the cell where it can disrupt enzymatic systems and damage mitochondria function. It also destroys hepatocytes (liver metabolic cells) (7). Let’s remember that sucralose was designed for an insecticide, never as a food product.

Chlorine is classified as a halide and like other halides like bromine and fluorine are highly reactive and can easily displace the only halide essential to our health…iodine. Iodine is required to make thyroid hormone, thyroxine (T4) and triiodothyronine (T3); in fact those numbers in T3 and T4 represent the number of iodine molecules in their respective hormone. If iodine gets displaced by these other halides, thyroid hormone becomes deficient leading to low thyroid function (8). Having a low functioning thyroid leads to many health issues including a sluggish metabolic rate and weight gain. When you consider the extensive usage of bromine in baked goods and breads (which gives the browning effect in buns and rolls), the fluorine in the drinking water, and that the most widely used AS is sucralose, it’s not a far stretch to see why many people suffer from low thyroid.

Just to note, the reason why cyclamate was banned was it caused bladder cancer in rats which violated the Delaney Clause. The Delaney Clause was set up in 1958 for the purpose of banning any food product that induced cancer in man or in lab animals (1). Yet, the FDA, has allowed the class-one carcinogen chlorine-enriched sucralose as well as the methanol-enriched aspartame and neotame freely into our food supply. It appears that the government picks and chooses which laws it will and will not enforce.

Conclusion
I have only touched upon a few artificial sweeteners, there are more, and more can be expected. The “References” section delves deeper into the pernicious practice of AS including the chemistry, the adverse effects and the politics (which are integral) associated with it.
To summarize here are just some of the signs and symptoms from AS usage:

Altered brain chemistry

Mood swings

Anxiety

Endocrine disruptor

Poor Sleep

Headaches

Joint and bone health

Metabolic disturbances

Visual abnormalities

Impaired thyroid

Anemia

Neurodegenerative problems

Tremors

Loss of life

Many of these findings indirectly cause weight gain. It also has been shown that AS consumption directly led to insulin and leptin resistance, the two hormones most responsible for weight gain (1).

The “food” chemists remain diligent in making us addicted to sweets. They fully realize that once they hijack your palate, they have lifetime customers. They fully realize that when the battle is drawn between one’s obsession with weight versus the chemical addiction to sweets, it is a gross mismatch, a no brainer, one that you can chalk up for the addicted side.

We know that sugar and AS consumption is the reason why nearly two-thirds of the population is overweight, which is three times (300%) more than just 20 years ago. Using history as our guide we can accurately assess that these numbers will steadily climb and that food manufacturers, advertisers and skilled “food” chemists, and our government will continue to do what they do best…mislead the public while making huge profit. It is no more complicated than if you want to lose weight you must be diligent in stabilizing your blood sugar and be obsessive in rejecting these harmful artificial sweeteners.

1 Comment

Roger Mason
March 28, 2014

Thank you for your comprehensive yet understandable article explaining the history and facts about artificial sweeteners. I had no idea of the extent of the possible side effects of the most common ones. I also never knew the difference between grain alcohol and wood alcohol, the devastating results of ingesting the latter, nor the range of the unintended consequences generated by Prohibition.

In the future I will steer clear of any products listing artificial sweeteners as an ingredient because now I know the truth…”Generally Regarded As Safe”…NOT!